Microsomal oxidation of praziquantel.
The metabolism of the non-labelled and 14C-labelled anthelmintic drug, praziquantel (PZQ; CAS 55268-74-1) was investigated by means of microsomal oxidation with rat liver homogenates. The metabolites formed were determined with linear thin-layer chromatography (TLC) radioactivity scanner after TLC separation, separated with TLC and analysed with high-pressure liquid chromatography and mass spectrometry method. The amounts and properties of the formed metabolites were described. It was stated that after microsomal oxidation monohydroxylated PZQ derivatives were obtained in greatest amount; the main fraction formed (35%) contained 4-OH-PZQ derivate which consisted of 80% cis-4-OH-PZQ and 20% of trans-4-OH-PZQ.
Högemann
A
A
Institut für Pharmazeutische Chemie, Universität Münster, Fed. Rep. of Germany.
Kiec-Kononowicz
K
K
Westhoff
F
F
Blaschke
G
G
D000818:Animals; D002845:Chromatography; D002851:Chromatography, High Pressure Liquid; D002855:Chromatography, Thin Layer; D066298:In Vitro Techniques; D008297:Male; D013058:Mass Spectrometry; D008862:Microsomes, Liver / Q000378:metabolism*; D008968:Molecular Conformation; D010084:Oxidation-Reduction; D011223:Praziquantel / Q000031:analogs & derivatives / Q000378:metabolism*; D051381:Rats; D011919:Rats, Inbred Strains
C067550:4-hydroxypraziquantel; D011223:Praziquantel